NF-56-EJ40 是一种有效，高亲和力和高度选择性的人 SUCNR1 (GPR91) 拮抗剂，IC₅₀ 为 25 nM，K_i 为 33.5 nM，对大鼠 SUCNR1 几乎没有活性。 NF-56-EJ40 对人源化大鼠 SUCNR1 具有高亲和力，K_i 值为 17.4 nM。

NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC 50 of 25 nM and a K i of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a K i value of 17.4 nM.

Solid

SUCNR1 (GPR91)

NF-56-EJ40 is bound deep inside the hydrophobic pocket, with the acid group coordinated by the hydroxyl groups of the conserved residues Y83 and Y30 on one side, and R281 on the other side. The conserved E18 is predicted to form an additional hydrogen bond to the piperazine ring of NF-56-EJ40. E22 and N274 in human SUCNR1 are replaced by K181.31 and K269 in rat SUCNR1. These two amino acid exchanges could prevent the binding of NF-56-EJ40 to rat SUCNR1 owing to steric hindrance. Radioligand-binding studies with human SUCNR1 showed partial agreement with our homology model: the Y30F mutant of human SUCNR1, shows reduced binding of NF-56-EJ40. Similar effects are observed with the E18K and E18R mutants, probably owing to steric clashes of the Lys and Arg residues with NF-56-EJ40 and the loss of a hydrogen bond to its piperazine ring.
Human SUCNR1 residues are introduced into

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Powder -20°C 3 years；4°C 2 years

[1]. Haffke M, et al. Structural basis of species-selective antagonist binding to the succinate receptor. Nature. 2019 Oct;574(7779):581-585.

In Vitro: DMSO : 5 mg/mL (11.27 mM; Need ultrasonic)H₂O : 4.55 mg/mL (10.26 mM; ultrasonic and adjust pH to 9 with NaOH)配制储备液